TP-5801 TFA
Based on 1 Customer Validation
TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.55%
- Fòrmula: C26H32BrF3N8O3
- Peso molecular:641.48
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 1.40 nM (TNK1)[1]
TP-5801 (10 pM-10 μM; 72 h) TFA treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) TFA inhibits TNK1-dependent L540 cell growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:10 pM-10 μM
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Incubation Time:72 hours
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Result:Inhibited TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against WT TNK1 and AAA mutant cells, respectively. Inhibited BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively.
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Cell Line:L540 cells
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Concentration:1, 10, 100, and 1000 nM
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Incubation Time:10 days
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Result:Inhibited TNK1-dependent L540 cell growth at low nM level.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) TFA treatment can inhibit localized tumor growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD/SCID mice injected with Ba/F3 luciferase cells expressing TNK1 AAA[1]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; once
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Result:Showed no signs of toxicity and significantly prolonged lifespan.
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Animal Model:NOD/SCID mice implanted subcutaneously with Ba/F3 luciferase cells expressing TNK1 AAA or BCR-ABL[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; 50 mg/kg; once daily; 7 days
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Result:Reduced phospho-STAT3 in TNK1-driven xenografts at 2 hours post-treatment, and tumor burden in mice xenografted.
Chemical Information
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Appearance Solid
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Peso molecular 641.48
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Fòrmula C26H32BrF3N8O3
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Color Light yellow to yellow
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SMILES
OC(C(F)(F)F)=O.CN1CCN(C2=C(C)C=C(NC3=NC=C(Br)C(NC4=CC=CN=C4N(C)C)=N3)C(OC)=C2)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 100 mg/mL (155.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5589 mL | 7.7945 mL | 15.5890 mL | 38.9724 mL |
| 5 mM | 0.3118 mL | 1.5589 mL | 3.1178 mL | 7.7945 mL | |
| 10 mM | 0.1559 mL | 0.7794 mL | 1.5589 mL | 3.8972 mL | |
| 15 mM | 0.1039 mL | 0.5196 mL | 1.0393 mL | 2.5982 mL | |
| 20 mM | 0.0779 mL | 0.3897 mL | 0.7794 mL | 1.9486 mL | |
| 25 mM | 0.0624 mL | 0.3118 mL | 0.6236 mL | 1.5589 mL | |
| 30 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2991 mL | |
| 40 mM | 0.0390 mL | 0.1949 mL | 0.3897 mL | 0.9743 mL | |
| 50 mM | 0.0312 mL | 0.1559 mL | 0.3118 mL | 0.7794 mL | |
| 60 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6495 mL | |
| 80 mM | 0.0195 mL | 0.0974 mL | 0.1949 mL | 0.4872 mL | |
| 100 mM | 0.0156 mL | 0.0779 mL | 0.1559 mL | 0.3897 mL |
TP-5801 TFA Related Classifications
HY-147316A Related Classifications
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